| 摘要 |
Novel avermectin and milbemycin compounds having the formula:
<CHEM>
in which the broken line indicates a single or double bond; R1 is hydrogen, oxo, lower alkanoyloxy, or hydroxy and is present only when the broken line indicates a single bond;
R2 is methyl, ethyl, isopropyl or sec-butyl; R3 is hydroxy, methoxy or lower alkanoyloxy;
R4 is hydrogen, hydroxy, lower alkanoyloxy, alpha -L-oleandrosyloxy, alpha -L-oleandrosyl- alpha -L-oleandrosyloxy, 4 min -loweralkanoyl- alpha -L-oleandrosyloxy, or 4 sec -loweralkonoyl-4 min - alpha -L-oleandrosyl- alpha -L-oleandrosyloxy; or are tri(lower alkyl)silyl protected hydroxy derivatives or pharmaceutically acceptable salts thereof. These compounds are prepared by oxidizing an avermectin or milbemycin compound. They have utility as anti-parasitic agents and may be made into compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests. |
